solidoralmodified-releasedosageformsanddrugdelivery1

8/11/2019 SolidOralModified-releaseDosageFormsandDrugDelivery1

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Solid Oral Modified-releaseDosage Forms and Drug

Delivery SystemsSan Pedro, BlessingSantos, Zelica Trina

So, Liza MarieTan, Alexis Vianca


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Modified Release

In recent years: use to describe dosage forms havingdrug release features based on time, course, and/orlocation that are designed to accomplish therapeutic orconvenience objectives not offered by conventional or

immediate-release forms USP differentiates modified-release forms as extended

release and delayed release.

Modified Release


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Delayed-release products

Enteric coated tablets or capsules

Designed to pass through the stomach unaltered, laterto release their medication within the intestinal tract

** enteric coatings- protect a subs. from destruction bygastric fluids or to reduce stomach distress caused byirritating drugs

Delayed-release and Extended-release Products


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Extended-release products

Designed to release their medication in a controlledmanner of a predetermined rate, duration and locationto achieve and maintain optimum therapeutic bloodlevels of drug

Delayed-release and Extended-release Products


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Most modified-release products are administered

orally (capsules and tablets). Some modified-release dosage forms and drug

delivery systems are described including:

Ocular

Parenteral Subdermal (transdermal patches)

Vaginal products


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Drugs that are not inherently long lasting and require

multiple daily dosing to achieve the desired therapeuticresults.

Multiple daily dosing is inconvenient for the patient andcan result in missed doses, madeup doses, andnoncompliance with the regimen.

When conventional immediate-release dosage forms aretaken on schedule and more than once daily, they causesequential therapeutic blood level peaks and valleysassociated with the taking of each dose.

The Rationale for Extended-releasePharmaceuticals


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When doses are not administered on schedule, the

resulting peaks and valleys reflect less than the optimumdrug therapy

If doses are administered too frequently, minimum toxicconcentrations of drug may be reached with toxic sideeffects resulting.

If doses are missed, periods of sub therapeutic drug bloodlevels or those below the minimum effective concentrationmay result, with no benefit to the patients.



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Extended-release tablets and capsule

Commonly taken only once or twice daily

Provide an immediate release of drug that promptlyproduces the desired therapeutic effect, followed bygradual release of additional amount of drug to maintain

this effect over a predetermined period* Sustained plasma drug levels

Eliminate the need for night dosing



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Non-oral rate-controlled drug delivery systems

Drug release patterno 24 hrs for most transdermal patches to 3 months for the

estradiol vaginal insert



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Less fluctuation in drug blood levels

-Controlling rate of release eliminates peaks and valleys of bloodlevels

Frequency reduction in dosing-extended release products frequently deliver more than asingle dose, hence may be taken less often than conventionalforms

Enhanced convenience and compliance- With less frequency of dosing a patient is less apt to neglecttaking a dose; also greater convenience with day and nightadministration

Advantages of Extended-ReleaseDosage Forms Over Conventional

Forms


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Reduction in adverse side effects

-Because of fewer blood level peaks outside therapeutic rangeand into toxic range, adverse side effects are less frequent

Reduction in overall health care costs

- Although initial cost of extended-release dosage forms may begreater than for conventional forms, overall cost of treatmentmay be less because of enhanced therapeutic benefit, fewerside effects, reduced time for healthcare personnel to dispenseand administer drugs and monitor patients

Advantages of Extended-ReleaseDosage Forms Over Conventional

Forms


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Loss of flexibility in adjusting the drug dose and/or

dosage regimen Sudden and total drug release

Dose dumping (failure to technology)

Disadvantages


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Many terms has been used by manufacturers to describe

product types and function.-Used to describe orally administered dosage forms Sustained Release (SR)

Sustained Action (SA)

Prolonged Action (PA)

Controlled Release (CR)

Extended Release (ER)

Timed Release (TR)

Long Acting (LA)

Terminology


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Sustained-release (SR)

- Designed to slowly release a drug in the body over anextended period of time

* Timed-release (TR)

- Consisting of a drug that is released in small amounts overtime usually in the gastrointestinal tract

* Sustained Action (SA)

- A drug product formulation that provides the required dosageinitially and then maintains or repeats it at desired intervals

Terminology


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Prolonged Action (PA)

- Designed to release drug slow and provide a backup drugcontinuously over a long interval of time, preventing rapidabsorption

* Controlled Release (CR)- Dosage forms of a drug that are released or are activated

over a period of time by controlled-release process or

technology* Long Acting (LA)

- Slowly effective after initial dosage but maintaining its effectsover a long period of time, being slowly absorbed and persistingin the tissues before being excreted

Terminology


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* Rate-controlled delivery

Applied to certain types of drug delivery systems inwhich the rate of delivery is controlled by features ofthe device rather than by physiologic or environmentalconditions

Like gastrointestinal pH or drug transit through thegastrointestinal tract

Terminology


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Extended-release (ER) designed to provide prolonged

release of the medication According to the U.S Food and Drug Administration:

- One that allows a reduction in dosing frequency from thatnecessitated by a conventional dosage form such as a solutionor an immediate-release dosage form

* Delayed Release- designed to release the drug at a timeother than promptly after administration The delayed may be time based or based on the influence of

environmental conditions, like gastrointestinal pH

Terminology


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Repeat Action

usually contain two single doses of medication, one forimmediate release and the second for delayed release.

Targeted Release

describes drug directed toward isolating or

concentrating a drug in a body region, tissue, or site forabsorption or for drug action

Terminology


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Examples of Extended-release


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Examples of Extended-release


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